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tadalafil, Cialis

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GENERIC NAME: tadalafil

BRAND NAME: Cialis

DRUG CLASS AND MECHANISM: Tadalafil is an oral drug that is used for treating impotence (the inability to attain or maintain a penile erection). It is in a class of drugs called phosphodiesterase inhibitors that also includes sildenafil (Viagra) and vardenafil (Levitra).

Erection of the penis is caused by the filling of the penis with blood. Filling occurs because the blood vessels that bring blood to the penis increase in size and deliver more blood to the penis, and, at the same time, the blood vessels that take blood away from the penis decrease in size and remove less blood from the penis.

Sexual stimulation that leads to an erection causes the production and release of nitric oxide in the penis. The nitric oxide causes an enzyme, guanylate cyclase, to produce cyclic guanosine monophosphate (cGMP). It is the cGMP that is primarily responsible for increasing and decreasing the size of the blood vessels carrying blood to and from the penis, respectively, and causing the erection. When the cGMP is destroyed by another enzyme, phosphodiesterase-5, the blood vessels return to their normal size, blood leaves the penis, and the erection ends. Tadalafil prevents phosphodiesterase-5 from destroying cGMP so that cGMP stays around longer. The persistence of cGMP leads to a more prolonged engorgement of the penis with blood.

Tadalafil was approved by the FDA in November 2003.

PRESCRIPTION: Yes.

GENERIC AVAILABLE: No.

PREPARATIONS: Tablets: 5, 10, and 20 mg.

STORAGE: Store at room temperature between 15-30 C (59-86 F).

PRESCRIBED FOR: Tadalafil is used for the treatment of impotence (erectile dysfunction, ED).

DOSING: For most individuals, the recommended starting dose of tadalafil is 10 mg per day taken before sexual activity. Depending on the adequacy of the response or side effects, the dose may be increased to 20 mg or decreased to 5 mg a day. The effect of tadalafil may last up to 36 hours. Individuals who are taking medications that increase the blood levels of tadalafil should not exceed a total dose of 10 mg in 72 hours (See drug interactions). Tadalafil may be taken with or without food since food does not affect its absorption from the intestine.

DRUG INTERACTIONS: The breakdown and elimination of tadalafil from the body may be decreased by erythromycin, ketoconazole (Nizoral), itraconazole (Sporanox), indinavir (Crixivan) and ritonavir (Norvir). Therefore, these drugs may increase the levels of tadalafil in the blood. If these drugs are being used at the same time as tadalafil, the dose of tadalafil should be reduced in order to avoid side effects from high levels of tadalafil.

Tadalafil exaggerates the increases in heart rate and lowering of blood pressure caused by nitrates, for example, nitroglycerin, isosorbide dinitrate (Isordil), isosorbide mononitrate (Imdur, Ismo, Monoket), nitroglycerin (Nitro-Dur, Transderm-Nitro) that are used primarily for treating heart pain (angina). In patients who take nitrates for angina, tadalafil could cause heart pain or possibly even a heart attack by exaggerating the increase in heart rate and the lowering of blood pressure. Therefore, tadalafil should not be used with nitrates.

Tadalafil also exaggerates the blood pressure lowering effects of some alpha-blocking drugs for example, terazosin (Hytrin) that primarily are used for treating high blood pressure or enlargement of the prostate. Individuals who take these alpha-blockers should be on a stable dose of the alpha-blocker before tadalafil is started. In such situations, tadalafil should be started at the lowest dose. If the patient is already taking tadalafil, the alpha-blocker should be started at the lowest dose. Tadalafil and alcohol both lower blood pressure. Therefore, combining tadalafil with alcohol may cause excessive drops in blood pressure and cause dizziness, headaches, and increased heart rate.




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